The method for preparing romidolipid liposome

A technology for romide liposide and romide liposome is applied in the field of preparing romide liposome liposomes to achieve the effects of prolonging administration time, reducing degradation and simple process

Active Publication Date: 2015-08-19
广州迈凯安生物医药研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, domestic research on romiglutin is almost blank

Method used

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  • The method for preparing romidolipid liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: See figure 1 , the present invention discloses a method for preparing romidolipid liposomes, comprising the following process:

[0036] Romiglutide liposome prescription:

[0037] Romiglutide

[0038] Preparation process of romiglutide liposome: Dissolve the prescription amount of soybean lecithin for injection, cholesterol, vitamin E and romiglutide in 1:1 chloroform-methanol and pour it into a pear-shaped bottle. Remove the organic solvent under reduced pressure in a water bath at 40°C, and form a uniform film on the bottle wall; dissolve the prescribed amount of sucrose in 100ml of phosphate buffer with a pH value of 6.8, pour it into a pear-shaped bottle, and use a rotary evaporator at 30rpm, Hydration is complete under 25°C water bath conditions; the obtained liposomes are passed through a high-pressure homogenizer, the pressure is 900 bar, and the number of cycles is 3 times to obtain liposomes with an average particle size of 108nm; the lipo...

Embodiment 2

[0039] Example 2: See figure 1 , the present invention discloses a method for preparing romidolipid liposomes, comprising the following process:

[0040] Romiglutide liposome prescription:

[0041] Romiglutide

[0042] Preparation process of romiglutide liposomes: Dissolve the prescription amount of soybean lecithin for injection, cholesterol, vitamin E and romiglutide in 1:3 chloroform-methanol and pour it into a pear-shaped bottle, and rotate the evaporator at 40rpm, Remove the organic solvent under reduced pressure in a water bath at 45°C, and form a uniform film on the bottle wall; dissolve the prescribed amount of sucrose in 150ml of phosphate buffer with a pH value of 6.8, pour it into a pear-shaped bottle, and use a rotary evaporator at 40rpm, Hydration is complete under 35°C water bath conditions, the obtained liposomes are passed through a high-pressure homogenizer, the pressure is 700bar, and the number of cycles is 5 times to obtain liposomes with an aver...

Embodiment 3

[0043] Example 3: See figure 1 , the present invention discloses a method for preparing romidolipid liposomes, comprising the following process:

[0044] Romiglutide liposome prescription:

[0045] Romiglutide

0.3g

Soybean Lecithin for Injection

5g

cholesterol

1g

sucrose

2g

Vitamin E

0.3g

Phosphate buffered saline with a pH of 6.8

200ml

[0046] Preparation process of romiglutide liposomes: dissolve the prescription amount of soybean lecithin for injection, cholesterol, vitamin E and romiglutide in 1:5 chloroform-methanol and pour it into a pear-shaped bottle. Remove the organic solvent under reduced pressure in a water bath at 50°C, and form a uniform film on the bottle wall; dissolve the prescribed amount of sucrose in 200ml of phosphate buffer with a pH value of 6.8, pour it into a pear-shaped bottle, and use a rotary evaporator at 50rpm, Hydration is complete under 45°C water bath conditions, the...

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Abstract

The invention discloses a method for preparing romidepsin lipidosome. The romidepsin lipidosome is prepared by using a film dispersion method through regarding cholesterol as a stabilizer, cane sugar as a cryoprotectant and vitamin E as an antioxidant, wherein the particle size of the lipidosome is made to be smaller than 120nm and the encapsulation efficiency is made to be greater than 85% by a high pressure homogenization method at the same time. The romidepsin lipidosome prepared by the method is capable of reducing the degradation of romidepsin, prolonging the administration time, improving the adaptability of patients, improving the targeting of romidepsin, increasing the anti-tumor effect, and reducing the toxic and side effects of drugs as all ingredients in the formula are physically compatible materials with high safety. Moreover, the method for preparing romidepsin lipidosome disclosed by the invention has the advantages of simple process and low cost, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a method for preparing romidipeptide liposomes. Background technique [0002] Romidepsin is a histone deacetylase (HDAC) inhibitor, which can cause histone hyperacetylation, thereby affecting the gene expression of cells. In some cancer cells, excessive Histone deacetylases inhibit the activation of genes that regulate normal cellular activity, so reduced activity of the enzyme activates these genes and causes cancer cell growth to slow or stop. [0003] Liposomes are multilayered vesicles formed when amphiphilic substances phospholipids and other amphoteric compounds such as cholesterol are dispersed in the water phase. Each layer is a lipid bilayer, and the interior of the vesicles is the water phase. The liposome structure has the characteristics of being suitable for in vivo degradation, non-toxic and non-immunogenic. A large number of experimental data prove t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/12A61K9/127A61P35/00
Inventor 肖文花安鸿江文敏
Owner 广州迈凯安生物医药研究院有限公司
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